ChemicalBook CAS DataBase List 107530-18-7

107530-18-7

Name	L-Threonine,(3R)-N-acetyl-3-hydroxy-L-leucyl-(aR)-a-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-3-hydroxy-4-methyl-1-oxo-2-[(1-oxopropyl)amino]pentyl]oxy]-L-leucyl-N,O-dimethyl-,(7(R)1)-lactone (9CI)
CAS	107530-18-7
Molecular Formula	C49H75N7O15
Molecular Weight	1002.16
MOL File	107530-18-7.mol

Chemical Properties

storage temp.	-20°C
solubility	Chloroform: soluble
form	Solid
color	Light yellow to brown

Safety Data

Symbol(GHS)	GHS02,GHS07
Signal word	Danger
Hazard statements	H225-H302+H312+H332-H319
Precautionary statements	P210-P233-P240-P241-P242-P243-P261-P264-P270-P271-P280-P301+P312-P303+P361+P353-P304+P340-P305+P351+P338-P321-P330-P362+P364-P337+P313-P370+P378-P403+P235-P501

Hazard Information

Uses

FR900359 is a depsipeptide selective inhibitor of Gαq/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research[1][2][3][4].

Definition

ChEBI: FR900359 is a cyclodepsipeptide.

in vivo

FR900359 (0.2 or 1 mg/ml, 12 μL per mouse, i.v.) strongly reduces vascular tone in mouse tail artery^[1].
FR900359 (0.1 mg/ml, 2.5 mg/mouse, intratracheally) abolishes airway hyperreactivity after Ovalbumin (HY-W250978)-induced sensitization in mice^[4].

Animal Model:	Isometric force measurements in mouse tail artery ^[1]
Dosage:	1.0 μM
Administration:	Washed
Result:	Strongly reduced vascular tone

Animal Model:	Ovalbumins–induced sensitization model of asthma. ^[4]
Dosage:	0.1 mg/ml, 2.5 mg per mouse
Administration:	Intratracheally
Result:	Abolished airway hyperreactivity after ovalbumin-induced sensitization in mice

storage

-20°C

References

[1] Schrage R, et.al. The experimental power of FR900359 to study Gq-regulated biological processes. Nat Commun. 2015 Dec 14;6:10156. DOI:10.1038/ncomms10156
[2] Fujioka, M,et.al. Structure of FR900359, a cyclic depsipeptide from Ardisia crenata sims J. Org. Chem. 1988, 53 (12), 2820?2825.
[3] Lapadula D, et.al. Effects of Oncogenic Gαq and Gα11 Inhibition by FR900359 in Uveal Melanoma. Mol Cancer Res. 2019 Apr;17(4):963-973. DOI:10.1158/1541-7786.MCR-18-0574
[4] Matthey M, et.al. Targeted inhibition of Gq signaling induces airway relaxation in mouse models of asthma. Sci Transl Med. 2017 Sep 13;9(407):eaag2288. DOI:10.1126/scitranslmed.aag2288

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